Literature DB >> 24685544

Identification of tertiary sulfonamides as RORc inverse agonists.

Benjamin P Fauber1, Olivier René2, Brenda Burton3, Christine Everett2, Alberto Gobbi2, Julie Hawkins3, Adam R Johnson2, Marya Liimatta2, Peter Lockey3, Maxine Norman3, Harvey Wong2.   

Abstract

Screening a nuclear receptor compound subset in a RORc biochemical binding assay revealed a benzylic tertiary sulfonamide hit. Herein, we describe the identification of compounds with improved RORc biochemical inverse agonist activity and cellular potencies. These improved compounds also possessed appreciable selectivity for RORc over other nuclear receptors.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Autoimmune; IL-17; Inflammation; RORc; RORγ

Mesh：

Substances：

Year:  2014        PMID： 24685544     DOI： 10.1016/j.bmcl.2014.03.038

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

1.  SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious RORγ Inhibitor.

Authors:  Kazuyuki Hirata; Masayuki Kotoku; Noriyoshi Seki; Takaki Maeba; Katsuya Maeda; Shintaro Hirashima; Takayuki Sakai; Shingo Obika; Akimi Hori; Yasunori Hase; Takayuki Yamaguchi; Yoshiaki Katsuda; Takahiro Hata; Naoki Miyagawa; Kojo Arita; Yukihiro Nomura; Kota Asahina; Yusuke Aratsu; Masafumi Kamada; Tsuyoshi Adachi; Masato Noguchi; Satoki Doi; Paul Crowe; Erin Bradley; Ruo Steensma; Haiyan Tao; Morgan Fenn; Robert Babine; Xiaolin Li; Scott Thacher; Hiromasa Hashimoto; Makoto Shiozaki
Journal:  ACS Med Chem Lett       Date:  2015-11-04       Impact factor: 4.345

2.  Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.

Authors:  Olivier René; Benjamin P Fauber; Gladys de Leon Boenig; Brenda Burton; Céline Eidenschenk; Christine Everett; Alberto Gobbi; Sarah G Hymowitz; Adam R Johnson; James R Kiefer; Marya Liimatta; Peter Lockey; Maxine Norman; Wenjun Ouyang; Heidi A Wallweber; Harvey Wong
Journal:  ACS Med Chem Lett       Date:  2014-12-04       Impact factor: 4.345

3.  Identification of an aminothiazole series of RORβ modulators.

Authors:  Rémi Patouret; Christelle Doebelin; Ruben D Garcia-Ordonez; Mi Ra Chang; Claudia Ruiz; Michael D Cameron; Patrick R Griffin; Theodore M Kamenecka
Journal:  Bioorg Med Chem Lett       Date:  2018-03-03       Impact factor: 2.823

Review 4.  ROR nuclear receptors: structures, related diseases, and drug discovery.

Authors:  Yan Zhang; Xiao-yu Luo; Dong-hai Wu; Yong Xu
Journal:  Acta Pharmacol Sin       Date:  2014-12-15       Impact factor: 6.150

5.  Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors.

Authors:  Yonghui Wang; Wei Cai; Yaobang Cheng; Ting Yang; Qian Liu; Guifeng Zhang; Qinghua Meng; Fangbin Han; Yafei Huang; Ling Zhou; Zhijun Xiang; Yong-Gang Zhao; Yan Xu; Ziqiang Cheng; Sijie Lu; Qianqian Wu; Jia-Ning Xiang; John D Elliott; Stewart Leung; Feng Ren; Xichen Lin
Journal:  ACS Med Chem Lett       Date:  2015-05-26       Impact factor: 4.345

Review 6.  (Inverse) Agonists of Retinoic Acid-Related Orphan Receptor γ: Regulation of Immune Responses, Inflammation, and Autoimmune Disease.

Authors:  Anton M Jetten; Donald N Cook
Journal:  Annu Rev Pharmacol Toxicol       Date:  2019-08-06       Impact factor: 13.820

7.  Retinoic acid-related Orphan Receptor γ (RORγ): connecting sterol metabolism to regulation of the immune system and autoimmune disease.

Authors:  Anton M Jetten; Yukimasa Takeda; Andrzej Slominski; Hong Soon Kang
Journal:  Curr Opin Toxicol       Date:  2018-02-01

8.  Retinoic Acid-Related Orphan Receptors (RORs): Regulatory Functions in Immunity, Development, Circadian Rhythm, and Metabolism.

Authors:  Donald N Cook; Hong Soon Kang; Anton M Jetten
Journal:  Nucl Receptor Res       Date:  2015-12-16
  8 in total

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